Ifenprodil-like NMDA receptor modulator based on the biphenyl scaffold

Nadezhda S. Temnyakova, Dmitry A. Vasilenko, Oleg I. Barygin, Mikhail Y. Dron, Elena B. Averina, Yuri K. Grishin, Vladimir V. Grigoriev, Vladimir A. Palyulin, Maxim V. Fedorov, Dmitry S. Karlov

    Research output: Contribution to journalArticlepeer-review

    2 Citations (Scopus)

    Abstract

    Ifenprodil-like NMDA receptor negative allosteric modulator based on the biphenyl scaffold has been identified using virtual screening. Docking approach demonstrated that the modulator maintains some characteristic interactions with protein similar to ifenprodil. Electrophysiological and radioligand investigations demonstrated the concentration-dependent NMDA/Gly-induced currents inhibition with IC50 = 5 μM and significant displacement of [H3]ifenprodil with EC50 = 30 μM, respectively.

    Original languageEnglish
    Pages (from-to)342-343
    Number of pages2
    JournalMendeleev Communications
    Volume30
    Issue number3
    DOIs
    Publication statusPublished - 1 May 2020

    Keywords

    • biphenyl scaffold
    • docking
    • electrophysiological investigations
    • negative allosteric modulator
    • NMDA receptors

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